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The Role of G Protein-coupled Receptor Kinases in Cancer
G protein-coupled receptors (GPCRs) are the largest family of plasma membrane receptors. Emerging evidence demonstrates that signaling through GPCRs affects numerous aspects of cancer biology such as vascular remolding, invasion, and migration. Therefore, development of GPCR-targeted drugs could pro...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Ivyspring International Publisher
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5821040/ https://www.ncbi.nlm.nih.gov/pubmed/29483837 http://dx.doi.org/10.7150/ijbs.22896 |
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author | Yu, Shan Sun, Litao Jiao, Yufei Lee, Leo Tsz On |
author_facet | Yu, Shan Sun, Litao Jiao, Yufei Lee, Leo Tsz On |
author_sort | Yu, Shan |
collection | PubMed |
description | G protein-coupled receptors (GPCRs) are the largest family of plasma membrane receptors. Emerging evidence demonstrates that signaling through GPCRs affects numerous aspects of cancer biology such as vascular remolding, invasion, and migration. Therefore, development of GPCR-targeted drugs could provide a new therapeutic strategy to treating a variety of cancers. G protein-coupled receptor kinases (GRKs) modulate GPCR signaling by interacting with the ligand-activated GPCR and phosphorylating its intracellular domain. This phosphorylation initiates receptor desensitization and internalization, which inhibits downstream signaling pathways related to cancer progression. GRKs can also regulate non-GPCR substrates, resulting in the modulation of a different set of pathophysiological pathways. In this review, we will discuss the role of GRKs in modulating cell signaling and cancer progression, as well as the therapeutic potential of targeting GRKs. |
format | Online Article Text |
id | pubmed-5821040 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | Ivyspring International Publisher |
record_format | MEDLINE/PubMed |
spelling | pubmed-58210402018-02-26 The Role of G Protein-coupled Receptor Kinases in Cancer Yu, Shan Sun, Litao Jiao, Yufei Lee, Leo Tsz On Int J Biol Sci Review G protein-coupled receptors (GPCRs) are the largest family of plasma membrane receptors. Emerging evidence demonstrates that signaling through GPCRs affects numerous aspects of cancer biology such as vascular remolding, invasion, and migration. Therefore, development of GPCR-targeted drugs could provide a new therapeutic strategy to treating a variety of cancers. G protein-coupled receptor kinases (GRKs) modulate GPCR signaling by interacting with the ligand-activated GPCR and phosphorylating its intracellular domain. This phosphorylation initiates receptor desensitization and internalization, which inhibits downstream signaling pathways related to cancer progression. GRKs can also regulate non-GPCR substrates, resulting in the modulation of a different set of pathophysiological pathways. In this review, we will discuss the role of GRKs in modulating cell signaling and cancer progression, as well as the therapeutic potential of targeting GRKs. Ivyspring International Publisher 2018-02-05 /pmc/articles/PMC5821040/ /pubmed/29483837 http://dx.doi.org/10.7150/ijbs.22896 Text en © Ivyspring International Publisher This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY-NC) license (https://creativecommons.org/licenses/by-nc/4.0/). See http://ivyspring.com/terms for full terms and conditions. |
spellingShingle | Review Yu, Shan Sun, Litao Jiao, Yufei Lee, Leo Tsz On The Role of G Protein-coupled Receptor Kinases in Cancer |
title | The Role of G Protein-coupled Receptor Kinases in Cancer |
title_full | The Role of G Protein-coupled Receptor Kinases in Cancer |
title_fullStr | The Role of G Protein-coupled Receptor Kinases in Cancer |
title_full_unstemmed | The Role of G Protein-coupled Receptor Kinases in Cancer |
title_short | The Role of G Protein-coupled Receptor Kinases in Cancer |
title_sort | role of g protein-coupled receptor kinases in cancer |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5821040/ https://www.ncbi.nlm.nih.gov/pubmed/29483837 http://dx.doi.org/10.7150/ijbs.22896 |
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